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Nuclear Receptors: From Structure to the Clinic

  • Iain J. McEwan
  • Raj Kumar

Table of contents

  1. Front Matter
    Pages i-xi
  2. Allosteric Regulation and Nuclear Receptor Complex Dynamics

    1. Front Matter
      Pages 15-15
    2. Peter J. Fuller, Jun Yang, Morag J. Young
      Pages 17-39
    3. Raj Kumar, Iain J. McEwan
      Pages 41-57
    4. Vanessa Dubois, Christine Helsen, Liesbeth Clinckemalie, Lien Spans, Michaël Laurent, Leen Antonio et al.
      Pages 59-72
    5. Jordan T. White, Hesam N. Motlagh, Jing Li, E. Brad Thompson, Vincent J. Hilser
      Pages 73-91
    6. Marek Orłowski, Piotr Dobryszycki, Anna Zoglowek, Joanna Pieprzyk, Katarzyna Bielska, Beata Greb-Markiewicz et al.
      Pages 93-117
    7. Brice Beinsteiner, Dino Moras
      Pages 119-133
  3. Nuclear Receptor Co-regulatory Protein Interactions

  4. Taking Nuclear Receptor Structure into the Clinic

  5. Back Matter
    Pages 229-236

About this book

Introduction

Nuclear Receptors focuses on the structural analysis of nuclear receptors from the initial work using isolated protein domains to the more recent exciting developments investigating the conformational shape of full-length receptor complexes. The book also reviews the structure of key nuclear receptor co-regulatory proteins. The aim is to bring together, for the first time, a comprehensive review of nuclear receptor structure and the importance of receptor conformation underpinning allosteric regulation by different ligands (hormone, drugs, DNA response elements, protein-protein interactions) and receptor activity.

The nuclear receptor superfamily, including receptors for steroid hormones and non-steroid ligands, are pivotal to normal physiology, regulating processes as diverse as reproduction, metabolism, the immune system and brain development. The first members of the family were cloned over 25 years ago, which heralded in the idea of a superfamily of intracellular receptor proteins that bound small molecule ligands: classical steroid hormones, vitamins, fatty acids and other products of metabolism. These signals are then transmitted through multiprotein receptor-DNA complexes, leading to the regulation of target genes, often in a cell-selective manner. The cloning of the receptor cDNAs also ushered in an era of unparalleled analysis of the mechanisms of action of these ligand-activated transcription factors.

Keywords

NMR spectroscopy glucocorticoids ligands nuclear receptors protein interactions selective androgen receptor modulators selective estrogen receptor modulators steroid hormones

Editors and affiliations

  • Iain J. McEwan
    • 1
  • Raj Kumar
    • 2
  1. 1.School of Medical SciencesUniversity of AberdeenAberdeenUnited Kingdom
  2. 2.Department of Basic SciencesThe Commonwealth Medical CollegeScrantonUSA

Bibliographic information